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Ezetimibe (brand name Zetia or Ezetrol) is a medication used to reduce high cholesterol levels in your blood. It comes as a tablet taken by mouth and works by reducing the amount of cholesterol your body absorbs from your digestive system, reducing the amount of cholesterol in the body. It is rarely prescribed alone and more commonly used in combination treatments with drugs known as statins or HMG reductase inhibitors (such as atorvastatin, simvastatin, and rosuvastatin), which are also used for reducing high cholesterol (Rosenson, 2020).
What is ezetimibe used for?
High cholesterol has long been known to be a problem, but if you thought it was just something you had to watch out for in your food, you’d be wrong. In fact, our bodies produce cholesterol, and it plays a lot of important roles, including in digesting our food, absorbing vitamins, building our cells, and producing hormones that help our organs communicate and work properly. That’s right. Not all cholesterol is bad.
Cholesterol travels in our bodies in different forms, and certain forms (like LDL, which is the “bad” kind) tend to leave bits of fat throughout our blood vessels as they travel through the bloodstream. This fat can build up and cause damage, blocking our blood vessels and preventing blood from flowing properly, resulting in conditions like heart attacks and strokes (Huff, 2020).
What is the mechanism of action?
Scientists have proven that reducing levels of LDL cholesterol in your blood plays a huge role in preventing conditions like stroke and heart attack. One study showed that patients at high risk who lowered their cholesterol using certain medications had a 28% lower risk of dying during the study than people who didn’t. Patients taking a combination of ezetimibe and statins have shown to have a lower risk of heart attack or stroke than patients just taking statins (Vallejo-Vez, 2017).
While statins alone are the most commonly prescribed medications for lowering LDL cholesterol, the second most common drug prescribed is ezetimibe. Treatment with just statins (monotherapy) requires higher doses, increasing the risk of side effects. Combining the two medications allows healthcare professionals to prescribe lower doses of statin drugs and avoid the side effects of using high doses of statins (such as muscle damage) (Rosenson, 2020).
It’s important to know that cholesterol-lowering medications are most effective when combined with a cholesterol-lowering diet. Research has shown that adopting a diet rich in fruits and vegetables can significantly reduce a person’s risk of developing cardiovascular disease (such as stroke and heart attack) (Sotos-Prieto, 2015). In addition, smoking or using tobacco products, as well as lack of physical activity, can contribute to high cholesterol and cardiovascular disease.
What are the side effects of ezetimibe?
Overall, ezetimibe is well-tolerated. The most commonly reported side effects among people taking ezetimibe include (MedLine Plus, 2020):
- Unusual tiredness
- Muscle aches
- Joint pain
There are additional side effects that may occur when taking this medication. The muscle aches associated with this drug are typically more severe when combined with a statin drug (such as atorvastatin). These combination medications that contain both ezetimibe and a statin medication include brand names such as Liptruzet and Atozet, among others (MedLine Plus, 2020).
How to lower cholesterol: medication and lifestyle
Serious side effects
Serious side effects are rare, but can happen, including (MedLine Plus, 2020)
- Muscle damage: Ezetimibe, especially when combined with a statin drug (like simvastatin or atorvastatin, such as in the combination medications Vytorin and Liptruzet) can increase the risk of muscle damage. While this typically causes only mild muscle pain, in rare cases, the muscle damage may be severe and result in a condition called rhabdomyolysis (which is the breakdown of the muscles and release of the byproducts into the bloodstream). Symptoms of rhabdomyolysis include severe muscle pain and weakness and dark urine. This condition can cause kidney problems if left untreated. If you develop these symptoms, seek immediate medical attention.
- Elevated liver enzymes: Your healthcare provider may perform a simple blood test before you begin this medication, as in some cases, it can cause an increase in liver markers. For the most part, this condition does not cause any problems; however, your healthcare provider may decide to stop using this medication if this occurs.
- In patients with severe kidney problems such as kidney failure, this medication remains in the body at higher levels, increasing the risk of serious side effects from the drug. If you have kidney disease, your healthcare provider should monitor you for side effects such as muscle pain, which is more common in patients taking certain lipid-lowering drugs who have kidney problems.
- In patients with liver disease, this drug is not removed as efficiently from the body. As a result, these patients may have higher levels of the drug in their bodies than other patients taking the same dose, increasing the risk of side effects such as muscle damage. Tell your healthcare provider if you have ever had liver problems.
What are the warnings?
Ezetimibe is not recommended for use by women who are breastfeeding or pregnant. Consult a healthcare professional if you are nursing or pregnant or plan to become pregnant to find an alternative option for controlling your cholesterol. Your healthcare provider may also monitor your liver function while you’re taking ezetimibe since some people have been found to have elevated levels of certain liver enzymes while taking it.
Since this medication is broken down by your liver, if you are found to have a liver problem, your healthcare provider may recommend using a different medication. The same is true for people with reduced kidney function. Your healthcare provider will likely reduce the dosage of your ezetimibe and monitor you for any problems (Rosenson, 2020).
Taking ezetimibe in combination with cholesterol-lowering drugs called fibrates (such as gemfibrozil) can result in the development of bile stones. While this condition can be asymptomatic, it can cause upper abdominal pain if the stones block your bile duct, especially after eating meals high in fat.
Do not take ezetimibe if you have ever had an allergic reaction to this medication. Before you begin taking ezetimibe, your healthcare provider may check your blood lipid levels and check them again as you continue your treatment.
Atorvastatin: what’s the right dosage for me?
Some people are also prescribed medications known as bile acid sequestrants, like cholestyramine (brand name Prevalite), colestipol (brand names Colestid and Colestipid), or colesevelam (brand name Welchol). These medications can reduce your body’s ability to absorb ezetimibe, so your healthcare provider will instruct you to take ezetimibe either more than two hours before the bile sequestrant or four hours after (MedLine Plus, 2020). Let your healthcare provider know if you are taking any herbal products or supplements as these can interfere with the medication you’ve been prescribed.
Dosing and cost
Ezetimibe is available as a pill taken once daily by mouth at a dosage of 10 mg. Ezetimibe and brand name Zetia are available for between $10–$30 for a 30 day supply (GoodRx, n.d.).
- GoodRx: Ezetimibe Prices, Coupons & Savings Tips. (n.d.). Retrieved September 16, 2020, from https://www.goodrx.com/ezetimibe
- Huff, T. (2020, April 15). Physiology, Cholesterol. Retrieved August 31, 2020, from https://www.ncbi.nlm.nih.gov/books/NBK470561/
- MedLine Plus. (2020). Ezetimibe. Retrieved from https://medlineplus.gov/druginfo/meds/a603015.html
- Rosenson, R. S. (2020, June 02). Low density lipoprotein cholesterol lowering with drugs other than statins and PCSK9 inhibitors. Retrieved August 30, 2020, from https://www.uptodate.com/contents/low-density-lipoprotein-cholesterol-lowering-with-drugs-other-than-statins-and-pcsk9-inhibitors?search=ezetimibe
- Sotos-Prieto, M., Bhupathiraju, S. N., Mattei, J., Fung, T. T., Li, Y., Pan, A. Hu, F. B. (2015). Changes in Diet Quality Scores and Risk of Cardiovascular Disease Among US Men and Women. Circulation, 132(23), 2212-2219. doi: 10.1161/circulationaha.115.017158. Retrieved from https://pubmed.ncbi.nlm.nih.gov/26644246/
- Vallejo-Vaz, A. J., Robertson, M., Catapano, A. L., Watts, G. F., Kastelein, J. J., Packard, C. J., Ray, K. K. (2017). Low-Density Lipoprotein Cholesterol Lowering for the Primary Prevention of Cardiovascular Disease Among Men With Primary Elevations of Low-Density Lipoprotein Cholesterol Levels of 190 mg/dL or Above. Circulation, 136(20), 1878-1891. doi: 10.1161/circulationaha.117.027966. Retrieved from https://www.ahajournals.org/doi/10.1161/CIRCULATIONAHA.117.027966
Dr. Mike is a licensed physician and the Director, Medical Content & Education at Ro.